Description: Selective, high affinity M2 antagonist
Chemical Name: 11-[[4-[4-(Diethylamino)butyl]-1-piperidinyl]acetyl]-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one
Purity: ≥99% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
High affinity, selective muscarinic M2 receptor antagonist (pKi values are 8.3, 7.7 and 6.82 for M2, M1 and M3 receptors, respectively). Displays cardioselectivity in vivo, over intestinal, tracheal and bladder muscarinic receptors; inhibits vagally and agonist-induced bradycardia.
Compound Libraries
AQ-RA 741 is also offered as part of the
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The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
1eq. HCl
46.36
100
DMSO
46.36
100
ethanol
46.36
100
Preparing Stock Solutions
The following data is based on the product molecular weight 463.62. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass
1 mg
5 mg
10 mg
1 mM
2.16 mL
10.78 mL
21.57 mL
5 mM
0.43 mL
2.16 mL
4.31 mL
10 mM
0.22 mL
1.08 mL
2.16 mL
50 mM
0.04 mL
0.22 mL
0.43 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Doodset al (1991) Cardioselectivity of AQ-RA 741, a novel tricyclic antimuscarinic drug. Eur.J.Pharmacol. 192 147 PMID: 2040358
Dorjeet al (1991) Antagonist binding profiles of five cloned human muscarinic receptor subtypes. J.Pharmacol.Exp.Ther. 256 727 PMID: 1994002
Doodset al (1994) Pharmacological profile of selective muscarinic receptor antagonists on guinea-pig ileal smooth muscle. Eur.J.Pharmacol. 253 275 PMID: 8200421